JP2003513066A5 - - Google Patents
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- Publication number
- JP2003513066A5 JP2003513066A5 JP2001534764A JP2001534764A JP2003513066A5 JP 2003513066 A5 JP2003513066 A5 JP 2003513066A5 JP 2001534764 A JP2001534764 A JP 2001534764A JP 2001534764 A JP2001534764 A JP 2001534764A JP 2003513066 A5 JP2003513066 A5 JP 2003513066A5
- Authority
- JP
- Japan
- Prior art keywords
- groups
- alkyl
- different
- formula
- aryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000004432 carbon atoms Chemical group C* 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 9
- 150000003839 salts Chemical class 0.000 description 9
- 239000011780 sodium chloride Substances 0.000 description 9
- 125000001424 substituent group Chemical group 0.000 description 7
- 125000003118 aryl group Chemical group 0.000 description 6
- 229910052739 hydrogen Inorganic materials 0.000 description 6
- 239000001257 hydrogen Substances 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- -1 nitro, hydroxy Chemical group 0.000 description 6
- 229910052757 nitrogen Inorganic materials 0.000 description 6
- 125000004433 nitrogen atoms Chemical group N* 0.000 description 6
- 125000000217 alkyl group Chemical group 0.000 description 5
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 125000005842 heteroatoms Chemical group 0.000 description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 4
- 125000002950 monocyclic group Chemical group 0.000 description 4
- 125000005915 C6-C14 aryl group Chemical group 0.000 description 3
- 229910052799 carbon Inorganic materials 0.000 description 3
- 125000000623 heterocyclic group Chemical group 0.000 description 3
- 150000002431 hydrogen Chemical class 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- 239000011593 sulfur Substances 0.000 description 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 150000002829 nitrogen Chemical group 0.000 description 2
- 230000000269 nucleophilic Effects 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 description 1
- 0 *C(C(CN(C(NI)=NI)I)N)=O Chemical compound *C(C(CN(C(NI)=NI)I)N)=O 0.000 description 1
- 108010054265 Factor VIIa Proteins 0.000 description 1
- 229940012414 Factor VIIa Drugs 0.000 description 1
- 108010074860 Factor Xa Proteins 0.000 description 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000005755 formation reaction Methods 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- OZAIFHULBGXAKX-UHFFFAOYSA-N precursor Substances N#CC(C)(C)N=NC(C)(C)C#N OZAIFHULBGXAKX-UHFFFAOYSA-N 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 200000000008 restenosis Diseases 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 201000011528 vascular disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99121623.5 | 1999-10-30 | ||
| EP99121623A EP1095933A1 (en) | 1999-10-30 | 1999-10-30 | Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them |
| PCT/EP2000/010395 WO2001032611A1 (en) | 1999-10-30 | 2000-10-21 | N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003513066A JP2003513066A (ja) | 2003-04-08 |
| JP2003513066A5 true JP2003513066A5 (ko) | 2007-12-06 |
| JP4658430B2 JP4658430B2 (ja) | 2011-03-23 |
Family
ID=8239305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001534764A Expired - Fee Related JP4658430B2 (ja) | 1999-10-30 | 2000-10-21 | Ｎ−グアニジノアルキルアミド、その製造、その使用およびそれを含む医薬調製物 |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US6472562B1 (ko) |
| EP (2) | EP1095933A1 (ko) |
| JP (1) | JP4658430B2 (ko) |
| KR (1) | KR100981593B1 (ko) |
| CN (1) | CN1249026C (ko) |
| AR (1) | AR026257A1 (ko) |
| AT (1) | ATE264837T1 (ko) |
| AU (1) | AU776797B2 (ko) |
| BR (1) | BR0015186A (ko) |
| CA (1) | CA2389412C (ko) |
| CZ (1) | CZ301855B6 (ko) |
| DE (1) | DE60010113T2 (ko) |
| DK (1) | DK1228039T3 (ko) |
| EE (1) | EE05168B1 (ko) |
| ES (1) | ES2220553T3 (ko) |
| HK (1) | HK1050673A1 (ko) |
| HR (1) | HRP20020372B1 (ko) |
| HU (1) | HUP0203627A3 (ko) |
| IL (2) | IL149209A0 (ko) |
| ME (1) | MEP54708A (ko) |
| MX (1) | MXPA02003805A (ko) |
| NO (1) | NO328016B1 (ko) |
| NZ (1) | NZ518607A (ko) |
| PL (1) | PL203859B1 (ko) |
| PT (1) | PT1228039E (ko) |
| RS (1) | RS50471B (ko) |
| RU (1) | RU2253651C2 (ko) |
| SI (1) | SI1228039T1 (ko) |
| SK (1) | SK286856B6 (ko) |
| TR (1) | TR200201181T2 (ko) |
| WO (1) | WO2001032611A1 (ko) |
| ZA (1) | ZA200203294B (ko) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1644401B1 (en) * | 2003-07-04 | 2011-03-09 | Lonza AG | Improved process for supported phase synthesis |
| CN102559644B (zh) | 2007-09-28 | 2015-03-25 | 普托拉制药有限公司 | 用于因子xa抑制剂的解毒剂和其使用方法 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| KR101897881B1 (ko) | 2008-01-04 | 2018-09-12 | 인텔리카인, 엘엘씨 | 특정 화학 물질, 조성물 및 방법 |
| NZ592837A (en) | 2008-11-14 | 2012-10-26 | Portola Pharm Inc | Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents |
| EP2414517B1 (en) * | 2009-03-30 | 2016-09-21 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same |
| JP6163304B2 (ja) * | 2009-07-15 | 2017-07-12 | ポートラ ファーマシューティカルズ， インコーポレイテッド | 第Ｘａ因子インヒビターの解毒剤の単位用量処方物およびその使用方法 |
| KR101875720B1 (ko) | 2011-01-10 | 2018-07-09 | 인피니티 파마슈티칼스, 인코포레이티드 | 이소퀴놀린온 및 이의 고체 형태의 제조 방법 |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| CN109640999A (zh) | 2016-06-24 | 2019-04-16 | 无限药品股份有限公司 | 组合疗法 |
| CN110357800B (zh) * | 2018-04-09 | 2022-07-26 | 青岛海生洋润生物科技有限公司 | 脯氨酸衍生物及其在制备治疗心脑血管疾病药物中的应用 |
| CN115317474A (zh) * | 2021-05-10 | 2022-11-11 | 中国海洋大学 | 一种苯酰胍衍生物在用于制备预防和治疗神经系统疾病或心血管系统疾病的药物中的应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5506134A (en) | 1990-10-22 | 1996-04-09 | Corvas International, Inc. | Hypridoma and monoclonal antibody which inhibits blood coagulation tissue factor/factor VIIa complex |
| US5788965A (en) | 1991-02-28 | 1998-08-04 | Novo Nordisk A/S | Modified factor VII |
| US5833982A (en) | 1991-02-28 | 1998-11-10 | Zymogenetics, Inc. | Modified factor VII |
| US5371072A (en) * | 1992-10-16 | 1994-12-06 | Corvas International, Inc. | Asp-Pro-Arg α-keto-amide enzyme inhibitors |
| DE4326465A1 (de) | 1993-01-20 | 1995-02-09 | Thomae Gmbh Dr K | Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
| EP0680682A1 (en) | 1993-01-20 | 1995-11-08 | ALEXANDROVICS, Peter, John | A line monitoring system |
| NZ263084A (en) * | 1993-03-12 | 1997-08-22 | Arris Pharm Corp | Dipeptide derivatives, treatment of immunomediated inflammatory disorders |
| SI9520044B (sl) | 1994-04-26 | 2004-08-31 | Aventis Pharmaceuticals Inc. | Inhibitorji Xa faktorja |
| US5869501A (en) * | 1994-12-02 | 1999-02-09 | Yamanouchi Pharmaceutical Co. Ltd | Amidinonaphthyl derivative or salt thereof |
| US6342504B1 (en) * | 1994-12-13 | 2002-01-29 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| AU8747598A (en) * | 1997-08-27 | 1999-03-16 | Kissei Pharmaceutical Co. Ltd. | 3-amidinoaniline derivatives, activated blood coagulation factor x inhibitors, and intermediates for producing both |
| SE9703414D0 (sv) * | 1997-09-23 | 1997-09-23 | Astra Ab | New compounds |
| WO1999033800A1 (en) | 1997-12-24 | 1999-07-08 | Aventis Pharma Deutschland Gmbh | Indole derivatives as inhibitors or factor xa |
| WO1999037643A1 (fr) * | 1998-01-26 | 1999-07-29 | Yamanouchi Pharmaceutical Co., Ltd. | Nouveaux derives heterocycliques a fusion benzenique ou sels de ceux-ci |
| EP0987274A1 (en) | 1998-09-15 | 2000-03-22 | Hoechst Marion Roussel Deutschland GmbH | Factor VIIa Inhibitors |
| JP2002543130A (ja) * | 1999-05-05 | 2002-12-17 | メルク エンド カムパニー インコーポレーテッド | 抗微生物剤としての新規なカテコール類 |
-
1999
- 1999-10-30 EP EP99121623A patent/EP1095933A1/en not_active Withdrawn
-
2000
- 2000-10-21 TR TR2002/01181T patent/TR200201181T2/xx unknown
- 2000-10-21 AT AT00971396T patent/ATE264837T1/de active
- 2000-10-21 PT PT00971396T patent/PT1228039E/pt unknown
- 2000-10-21 AU AU10265/01A patent/AU776797B2/en not_active Ceased
- 2000-10-21 HU HU0203627A patent/HUP0203627A3/hu unknown
- 2000-10-21 CN CNB008151407A patent/CN1249026C/zh not_active Expired - Fee Related
- 2000-10-21 ME MEP-547/08A patent/MEP54708A/xx unknown
- 2000-10-21 RS YUP-297/02A patent/RS50471B/sr unknown
- 2000-10-21 RU RU2002114041/04A patent/RU2253651C2/ru not_active IP Right Cessation
- 2000-10-21 CA CA002389412A patent/CA2389412C/en not_active Expired - Fee Related
- 2000-10-21 NZ NZ518607A patent/NZ518607A/en not_active IP Right Cessation
- 2000-10-21 BR BR0015186-6A patent/BR0015186A/pt active Search and Examination
- 2000-10-21 CZ CZ20021489A patent/CZ301855B6/cs not_active IP Right Cessation
- 2000-10-21 EP EP00971396A patent/EP1228039B1/en not_active Expired - Lifetime
- 2000-10-21 PL PL354808A patent/PL203859B1/pl not_active IP Right Cessation
- 2000-10-21 DK DK00971396T patent/DK1228039T3/da active
- 2000-10-21 ES ES00971396T patent/ES2220553T3/es not_active Expired - Lifetime
- 2000-10-21 MX MXPA02003805A patent/MXPA02003805A/es active IP Right Grant
- 2000-10-21 IL IL14920900A patent/IL149209A0/xx active IP Right Grant
- 2000-10-21 JP JP2001534764A patent/JP4658430B2/ja not_active Expired - Fee Related
- 2000-10-21 WO PCT/EP2000/010395 patent/WO2001032611A1/en active IP Right Grant
- 2000-10-21 SI SI200030422T patent/SI1228039T1/xx unknown
- 2000-10-21 SK SK578-2002A patent/SK286856B6/sk not_active IP Right Cessation
- 2000-10-21 DE DE60010113T patent/DE60010113T2/de not_active Expired - Lifetime
- 2000-10-21 EE EEP200200199A patent/EE05168B1/xx not_active IP Right Cessation
- 2000-10-26 AR ARP000105647A patent/AR026257A1/es active IP Right Grant
- 2000-10-27 US US09/697,188 patent/US6472562B1/en not_active Expired - Lifetime
-
2002
- 2002-04-18 IL IL149209A patent/IL149209A/en not_active IP Right Cessation
- 2002-04-25 ZA ZA200203294A patent/ZA200203294B/xx unknown
- 2002-04-26 HR HR20020372A patent/HRP20020372B1/xx not_active IP Right Cessation
- 2002-04-29 KR KR1020027005515A patent/KR100981593B1/ko not_active IP Right Cessation
- 2002-04-29 NO NO20022022A patent/NO328016B1/no not_active IP Right Cessation
- 2002-08-26 US US10/227,222 patent/US6664393B2/en not_active Expired - Lifetime
-
2003
- 2003-04-10 HK HK03102613A patent/HK1050673A1/xx not_active IP Right Cessation
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